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New Painkilling Drug Formula Targets Drug Overuse

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www.ProHealth.com • August 17, 2001




The popular pain relief medication OxyContin, has been increasingly abused among patients and recreational drug users and has prompted the drug’s producer Purdue Pharma, to develop a new formulation that includes a “sequestered antagonist,” which would work to prevent the medication’s abuse.

Peliminary research results appear to show some progress in the development of an abuse proof formula, according to Dr. Paul Goldenheim, Executive Vice President, Worldwide Research and Development.

"One of our recent efforts focuses on the use of an antagonist to block the effect of the opioid if it is abused," said Goldenheim. "When appropriately taken by a pain patient, the tablet is swallowed whole, and the antagonist should pass through the gastrointestinal system of a patient without significant release. Preliminary in vitro studies to date have demonstrated that the release of the antagonist from the intact dosage form is minimal (less than 5% of the total after 36 hours). When the dosage form is tampered, such as by crushing, in vitro results show that the entire amount of antagonist is released, thus potentially causing an undesirable effect to the abuser. If these results can be confirmed in clinical studies, this will be a significant technical achievement."

In its original time-release pill form, OxyContin is safe taken as prescribed. When abusers crush the pill they compromise this time-release delivery system and then sniff the powder or inject it to achieve a "high." In this form, the opiod drug is highly addictive.

“If this [new] tablet is abused, preliminary in vitro studies show that it behaves in a completely different way," Dr. Goldenheim continues. "Crushing the tablet to defeat its time-release properties also releases the antagonist, which blocks the effects of the opioid. Abusers will not experience euphoria and may experience the uncomfortable effects of withdrawal. We hope that knowledge of the tablet's abuse-resistant properties will deter potential drug abusers from even trying this product."

Jeffrey Lackner, Ph.D., a pain specialist at the University at Buffalo, warns that the potential for abuse of the original drug also is high among patients receiving the drug legitimately if they are not monitored closely by their physicians.

"Unfortunately, narcotics for chronic pain are, literally and figuratively, prescription for disaster if the physician neglects to consider abuse potential, history of self-medication, and other behavioral and psychological factors which bear on the trajectory of pain states," Lackner said.

"By the same token, patients who see 'oxy' as a 'cure' for an incurable problem without enhancing self-care skills can be a problem. This is particularly true with anxious pain patients who often misinterpret negative emotions for pain and ratchet up their use of drugs,” he said.



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